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09 Oct 17:28

[ASAP] Activating and Stabilizing Lattice Oxygen via Self-Adaptive Zn–NiOOH Sub-Nanowires for Oxygen Evolution Reaction

by Yuan Huang, Zeyu Wang, Hai Xiao, Qingda Liu, and Xun Wang

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Journal of the American Chemical Society
DOI: 10.1021/jacs.4c09931
09 Oct 15:13

Structural basis for Vipp1 membrane binding: from loose coats and carpets to ring and rod assemblies

by Benedikt Junglas

Nature Structural & Molecular Biology, Published online: 08 October 2024; doi:10.1038/s41594-024-01399-z

The authors present structures of endosomal sorting complexes required for transport III family member vesicle-inducing protein in plastids 1, ranging from helical assemblies and stacked rings to flat carpets, providing insights into transitions dependent on membrane tubulation and curvature needed for forming different architectures involved in membrane remodeling.
26 Dec 22:32

A pancreatic cancer organoid platform identifies an inhibitor specific to mutant KRAS

by Xiaohua Duan, Tuo Zhang, Lingling Feng, Neranjan de Silva, Benjamin Greenspun, Xing Wang, Jenna Moyer, M. Laura Martin, Rohit Chandwani, Olivier Elemento, Steven D. Leach, Todd Evans, Shuibing Chen, Fong Cheng Pan
Duan et al. developed a panel of isogenic murine pancreatic organoids containing common PDAC driver mutations to screen for KRAS mutation inhibitors and identified that perhexiline maleate can target KRAS mutation by downregulating the cholesterol biosynthesis pathway, which is specifically induced by KRAS mutation.
13 Oct 20:44

[ASAP] Identification of Bona Fide RNA Editing Sites: History, Challenges, and Opportunities

by Meng How Tan

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Accounts of Chemical Research
DOI: 10.1021/acs.accounts.3c00462
26 Apr 02:30

Design of Near‐Infrared Nonfullerene Acceptor with Ultralow Nonradiative Voltage Loss for High‐Performance Semitransparent Ternary Organic Solar Cells

by Wuyue Liu, Shaoming Sun, Liang Zhou, Yong Cui, Wenkai Zhang, Jianhui Hou, Feng Liu, Shengjie Xu, Xiaozhang Zhu
Design of Near-Infrared Nonfullerene Acceptor with Ultralow Nonradiative Voltage Loss for High-Performance Semitransparent Ternary Organic Solar Cells

An N-substituted asymmetric nonfullerene acceptor SN with an over 40 nm bathochromically shifted absorption compared to Y6 is designed and synthesized. The PM6 : SN-based binary cell exhibits the lowest nonradiative voltage loss of 0.15 eV ever achieved by organic solar cells (OSCs). Benefiting from extended NIR absorption and lowered voltage loss, PM6 : Y6 : SN-based semitransparent (ST)-OSCs, for the first time, achieve a power conversion efficiency of 14 % with an average visible transmittance over 20 %.


Abstract

Semitransparent organic solar cells (ST-OSCs) are considered as one of the most valuable applications of OSCs and a strong contender in the market. However, the optical band gap of current high-performance ST-OSCs is still not low enough to achieve the optimal balance between power conversion efficiency (PCE) and average visible transmittance (AVT). An N-substituted asymmetric nonfullerene acceptor SN with over 40 nm bathochromically shifted absorption compared to Y6 was designed and synthesized, based on which the device with PM6 as donor obtained a PCE of 14.3 %, accompanied with a nonradiative voltage loss as low as 0.15 eV. Meanwhile, ternary devices with the addition of SN into PM6 : Y6 can achieve a PCE of 17.5 % with an unchanged open-circuit voltage and improved short-circuit current. Benefiting from extended NIR absorption and lowered voltage loss, ST-OSCs based on PM6 : SN : Y6 were fabricated and the optimized device demonstrated a PCE of 14.0 % at an AVT of 20.2 %, which is the highest PCE at an AVT over 20 %.

21 Nov 09:08

[ASAP] Head to Tail Distortion Wave Characterizes the Enantiomerization of Helicenes

by Ariela W. Kaspi-Kaneti, Jorge Barroso, Gabriel Merino, David Avnir, Ignacio L. Garzón, and Inbal Tuvi-Arad

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The Journal of Organic Chemistry
DOI: 10.1021/acs.joc.0c02196
25 Dec 07:53

[ASAP] Isopimarane Diterpenoids from the Rhizomes of Kaempferia marginata and Their Potential Anti-inflammatory Activities

by Ratchanaporn Chokchaisiri*†, Waraluck Chaichompoo‡, Warangkana Chunglok§, Sarot Cheenpracha†, Lucksagoon Ganranoo†, Nathaporn Phutthawong†, Sareeya Bureekaew?, and Apichart Suksamrarn‡

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Journal of Natural Products
DOI: 10.1021/acs.jnatprod.9b00307
26 Oct 02:19

Catalytic Enantioselective Cyclopropenation of Internal Alkynes: Access to Difluoromethylated Three‐Membered Carbocycles

by Zhi-Qi Zhang, Meng-Meng Zheng, Xiao-Song Xue, Ilan Marek, Fa-Guang Zhang, Jun-An Ma
Angewandte Chemie International Edition Catalytic Enantioselective Cyclopropenation of Internal Alkynes: Access to Difluoromethylated Three‐Membered Carbocycles

Three's a crowd: A highly enantioselective RhII‐catalyzed cyclopropenation reaction of difluorodiazoethane (PhSO2CF2CHN2) with challenging internal alkynes is reported (up to 99 % yield, 97 % ee). Versatile stereoselective transformations of these unique strained cyclopropenes are also demonstrated.


Abstract

Herein we described an efficient RhII‐catalyzed enantioselective cyclopropenation reaction of internal alkynes with a masked difluorodiazoethane reagent (PhSO2CF2CHN2, Ps‐DFA). This asymmetric transformation offers efficient access to a broad range of enantioenriched difluoromethylated cyclopropenes (40 examples, up to 99 % yield, 97 % ee). The synthetic utility of obtained strained carbocycles is demonstrated by subsequent stereodefined processes, including cross‐couplings, hydrogenation, Diels–Alder reaction, and Pauson–Khand reaction.

27 Aug 01:29

Antiprotozoal alkaloid principles of the plant family Amaryllidaceae

Publication date: 15 October 2019

Source: Bioorganic & Medicinal Chemistry Letters, Volume 29, Issue 20

Author(s): Jerald J. Nair, Johannes van Staden

Abstract

Protozoan-borne diseases are prominent amongst diseases caused by parasites. Given their alarming morbidity and mortality statistics, there is ever growing interest in new therapies against these diseases. Whilst synthetic drugs such as benznidazole and melarsoprol have had a profound influence on the clinical setup, there has been significant interest in the phytochemical platform to also deliver such drug candidates. The plant family Amaryllidaceae is recognizable for its isoquinoline alkaloids, which exhibit attractive molecular architectures and interesting biological properties. This survey focuses on the antiprotozoal activities of 73 of such substances described in 18 different species of the Amaryllidaceae. Of these, 2-O-acetyllycorine was identified as the most potent (IC50 0.15 μg/mL against Trypansoma brucei brucei). Also considered are structure-activity relationships which have served to modulate activities, as well as the plausible mechanisms that underpin these effects and afford insight to the Amaryllidaceae alkaloid antiprotozoal pharmacophore.

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10 Apr 01:18

Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer

Publication date: 15 June 2019

Source: Bioorganic & Medicinal Chemistry Letters, Volume 29, Issue 12

Author(s): Kuojun Zhang, Yong Ni, Jiaxuan Chen, Zhengchao Tu, Xiaoxing Wu, Dong Chen, Hequan Yao, Sheng Jiang

Abstract

Nicotinamide phosphoribosyltransferase (NAMPT) has emerged as a promising target for the discovery of anticancer drugs. Based on NAMPT inhibitor FK866 that has been advanced into phase II trial, we identified a trans-3-(pyridin-3-yl)acrylamide compound 13 incorporating with a biarylsulfanilamide moiety as a new NAMPT inhibitor. Further structure-activity relationship (SAR) exploration led to additional biarylsulfanilamide-derived compounds with high in vitro NAMPT inhibitory potency and antiproliferative activity. In particular, compound 23, the most potent NAMPT inhibitor (IC50 = 5.08 nM), showed single-digit nanomolar antiproliferative activity against DU145, Hela, and H1975 cells with IC50 values of 2.90 nM, 2.34 nM, and 2.24 nM, respectively, and even subnanomolar level against K562, MCF-7, and HUH7 cells with IC50 values of 0.46 nM, 0.23 nM and 0.53 nM, respectively. Our findings provided promising lead compounds for the discovery of more potent NAMPT inhibitors as anticancer drugs.

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Graphical abstract for this article

26 Oct 14:21

[ASAP] Direct and Catalytic Amide Synthesis from Ketones via Transoximation and Beckmann Rearrangement under Mild Conditions

by Kengo Hyodo, Genna Hasegawa, Naoki Oishi, Kazuma Kuroda, Kingo Uchida

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The Journal of Organic Chemistry
DOI: 10.1021/acs.joc.8b01810
16 Oct 03:49

[ASAP] Mechanism for O–O Bond Formation via Radical Coupling of Metal and Ligand Based Radicals: A New Pathway

by Yulia Pushkar, Yuliana Pineda-Galvan, Alireza K. Ravari, Tatiana Otroshchenko, Daniel A. Hartzler

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Journal of the American Chemical Society
DOI: 10.1021/jacs.8b06836
07 Feb 01:26

Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives

Publication date: 15 February 2017
Source:Bioorganic & Medicinal Chemistry Letters, Volume 27, Issue 4
Author(s): Francisco G. Avalos-Alanís, Eugenio Hernández-Fernández, Pilar Carranza-Rosales, Susana López-Cortina, Jorge Hernández-Fernández, Mario Ordóñez, Nancy E. Guzmán-Delgado, Alejandro Morales-Vargas, Víctor M. Velázquez-Moreno, María G. Santiago-Mauricio
The synthesis of six α,β,-unsaturated amides and six 2,4-disubstituted oxazolines derivatives and their evaluation against two Mycobacterium tuberculosis strains (sensitive H37Rv and a resistant clinical isolate) is reported. 2,4-Disubstituted oxazolines (S)-3b,d,e were the most active in the sensitive strain with a MIC of 14.2, 13.6 and 10.8μM, respectively, and the compounds (S)-3d,f were the most active against resistant strain with a MIC of 6.8 and 7.4μM. The ex-vivo evaluation of hepatotoxicity on precision-cut rat liver slices was also tested for the α,β-unsaturated amides (S)-2b and (S)-2d,f and for the oxazolines (S)-3b and (S)-3d,f at different concentrations (5, 15 and 30μg/mL). The results indicate that these compounds possess promising antimycobacterial activity and at the same time are not hepatotoxic. These findings open the possibility for development of new drugs against tuberculosis.

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29 Dec 01:15

Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists

by Lai Wei, Jixia Wang, Xiuli Zhang, Ping Wang, Yaopeng Zhao, Jiaqi Li, Tao Hou, Lala Qu, Liying Shi, Xinmiao Liang and Ye Fang

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.6b01431
12 Apr 11:26

Synthesis of Lithium Boracarbonate Ion Pairs by Copper-Catalyzed Multi-Component Coupling of Carbon Dioxide, Diboron, and Aldehydes

Synthesis of Lithium Boracarbonate Ion Pairs by Copper‐Catalyzed Multi‐Component Coupling of Carbon Dioxide, Diboron, and Aldehydes

A novel family of well-defined molecular lithium boracarbonate ion pairs containing a unique boron-implanted cyclic carbonate framework are efficiently synthesized by the highly selective coupling reaction of CO2, bis(pinacolato)diboron, LiOtBu, and a wide range of aldehydes in the presence of an N-heterocyclic carbene copper catalyst.

[Communication]
Béatrice Carry, Liang Zhang, Masayoshi Nishiura, Zhaomin Hou
Angew. Chem. Int. Ed., April 09, 2016, DOI: 10.1002/anie.201602278. Read article